1A-116

SKU: orb1308731

Description

1A-116

Research Area

Cell Biology, Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 1430208-73-3
• MW: 307.31
• Purity: 99.71%
• Formula: C₁₆H₁₆F₃N₃
• SMILES: Cc1cc(C)cc(NC(=N)Nc2ccccc2C(F)(F)F)c1
• Target: Rho,Ras,Apoptosis
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (13.02 mM);DMSO:100 mg/mL (325.4 mM);H2O:< 0.1 mg/mL (insoluble)

Bioactivity

• Target IC50:
  Antiproliferative:4 µM(F3II cell)
• In Vivo:
  Daily treatment of mice with compound 1A-116 at 3mg/kg body weight/day reduces about 60% the formation of total metastatic lung colonies. A significant antitumor activity is obtained for macronodules (more than 1 mm in diameter) by treatment with 1A-116 in this highly aggressive breast cancer model. The treatment with 1A-116 reduces the total lung weight compare to the control group, leading to a total weight similar to the average pulmonary weight of Balb/c mice.
• In Vitro:
  1A-116 shows lesser effect on MCF7::pcDNA.3 cells than on MCF7::C1199 cells. 1A-116 treatment decreases phospho-PAK1 levels in a time-dependent manner. The presence of 1A-116 reverts the PAK1 phosphorylation induced by 4-hydroxytamoxifen (Tam). The presence of 1A-116 also effectively reverts Rac1-PAK1-mediated estrogen receptor (ER) phosphorylation at Ser305. 1A-116 shows a significant increase in antiproliferative activity on F3II cells, showing an IC50 value of 4 μM. A-116 also dramatically impairs Rac1 activation at low micromolar range (1 μM).

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Rho GTPases, Ras, TIAM1, Rac1, circadian rhythms, 1A116, 1A-116, 1A 116, Apoptosis, EGF, Inhibitor, inhibit

Compound Identifiers

PubChem CID

71543346